Abstract
The inhibition of D-glucose transport into brain by several hexose analogues has been investigated in adult anaesthetized rats. D-Glucose was transported with apparent Vmax. = 1.22 mumol/g per min, Km = 11.12 mM and Kd = 0.008 ml/g per min. 6-Chloro-6-deoxyglucose was transported with corresponding values of Vmax. = 1.33 mumol/g per min, Km = 5.5 mM and Kd = 0.0155 ml/g per min and inhibited D-glucose transport with apparent Ki = 3.01 mM. 6-Chloro-6-deoxymannose, 6-chloro-6-deoxygalactose and 6-tosyl-6-deoxygalactose also inhibited D-glucose transport, but 6-chloro-6-deoxyfructose was without effect. The results were consistent with a model for glucose transport at the blood/brain interface that involves a hydrophobic site on the transport protein at or near the 6-position of bound glucose.
Full text
PDFSelected References
These references are in PubMed. This may not be the complete list of references from this article.
- Bachelard H. S., Daniel P. M., Love E. R., Pratt O. E. The transport of glucose into the brain of the rat in vivo. Proc R Soc Lond B Biol Sci. 1973 Feb 27;183(1070):71–82. doi: 10.1098/rspb.1973.0005. [DOI] [PubMed] [Google Scholar]
- Barnett J. E., Holman G. D., Munday K. A. Structural requirements for binding to the sugar-transport system of the human erythrocyte. Biochem J. 1973 Feb;131(2):211–221. doi: 10.1042/bj1310211. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Betz A. L., Gilboe D. D., Drewes L. R. The characteristics of glucose transport across the blood brain barrier and its relation to cerebral glucose metabolism. Adv Exp Med Biol. 1976;69:133–149. doi: 10.1007/978-1-4684-3264-0_11. [DOI] [PubMed] [Google Scholar]
- Betz A. L., Gilboe D. D., Yudilevich D. L., Drewes L. R. Kinetics of unidirectional glucose transport into the isolated dog brain. Am J Physiol. 1973 Sep;225(3):586–592. doi: 10.1152/ajplegacy.1973.225.3.586. [DOI] [PubMed] [Google Scholar]
- Brown-Woodman P. D., Mohri H., Mohri T., Suter D., White I. G. Mode of action of alpha-chlorohydrin as a male anti-fertility agent. Inhibition of the metabolism of ram spermatozoa by alpha-chlorohydrin and location of block in glycolysis. Biochem J. 1978 Jan 15;170(1):23–37. doi: 10.1042/bj1700023. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Cremer J. E., Braun L. D., Oldendorf W. H. Changes during development in transport processes of the blood-brain barrier. Biochim Biophys Acta. 1976 Nov 2;448(4):633–637. doi: 10.1016/0005-2736(76)90120-6. [DOI] [PubMed] [Google Scholar]
- Crone C. Facilitated transfer of glucose from blood into brain tissue. J Physiol. 1965 Nov;181(1):103–113. doi: 10.1113/jphysiol.1965.sp007748. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Devés R., Krupka R. M. Testing transport models with substrates and reversible inhibitors. Biochim Biophys Acta. 1978 Oct 19;513(1):156–172. doi: 10.1016/0005-2736(78)90120-7. [DOI] [PubMed] [Google Scholar]
- Ford W. C., Harrison A., Waites G. M. Effects of the optical isomers of alpha-chlorohydrin on glycolysis by ram testicular spermatozoa and the fertility of male rats. J Reprod Fertil. 1977 Sep;51(1):105–109. doi: 10.1530/jrf.0.0510105. [DOI] [PubMed] [Google Scholar]
- Ford W. C., Waites G. M. A reversible contraceptive action of some 6-chloro-6-deoxy sugars in the male rat. J Reprod Fertil. 1978 Jan;52(1):153–157. doi: 10.1530/jrf.0.0520153. [DOI] [PubMed] [Google Scholar]
- Oldendorf W. H. Brain uptake of radiolabeled amino acids, amines, and hexoses after arterial injection. Am J Physiol. 1971 Dec;221(6):1629–1639. doi: 10.1152/ajplegacy.1971.221.6.1629. [DOI] [PubMed] [Google Scholar]
- Pardridge W. M., Oldendorf W. H. Kinetics of blood-brain transport of hexoses. Biochim Biophys Acta. 1975 Mar 25;382(3):377–392. doi: 10.1016/0005-2736(75)90279-5. [DOI] [PubMed] [Google Scholar]
- Reese T. S., Karnovsky M. J. Fine structural localization of a blood-brain barrier to exogenous peroxidase. J Cell Biol. 1967 Jul;34(1):207–217. doi: 10.1083/jcb.34.1.207. [DOI] [PMC free article] [PubMed] [Google Scholar]